COX
特异性亚型抑制剂
COX产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S1261 |
CelecoxibCelecoxib (SC 58635) 是一种选择性COX-2抑制剂,在Sf9细胞中IC50为40 nM。 |
![]() ![]() Reduced hepatic lipid contents and alleviated liver injury in EC-AMPK mice treated with selective COX-2 inhibitors. Wild-type and EC-AMPK mice given a high fat diet were treated with vehicle, celecoxib or nimesulide for a period of 4 weeks. At the end of treatment, parameters including body weight and circulating glucose (A), serum triglyceride and cholesterol levels (B were measured and presented as percentage comparisons against those from vehicle-treated wild-type mice. *P < 0.05 versus wild-type mice treated with vehicle; #P < 0.05 versus EC-AMPK mice treated with vehicle, n = 3-5. |
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S1396 |
ResveratrolResveratrol具有广泛靶点,包括环氧酶(如COX, IC50=1.1 μM)、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素,具有抗癌,抗炎,降血糖和其他有益心血管的作用。Resveratrol可诱导线粒体自噬、细胞自噬和自噬依赖性的凋亡。 |
![]() ![]() Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours. |
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S1255 |
NepafenacNepafenac (AHR 9434, AL 6515) 是一种非甾体抗炎药剂。 |
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S1638 |
IbuprofenIbuprofen 是一种抗炎类抑制剂,作用于COX-1和COX-2,IC50分别为13 μM和370 μM。 |
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S1723 |
IndomethacinIndomethacin是一种非选择性的COX1和COX2的抑制剂,IC50分别为0.1 μg/mL和5 μg/mL。常用于降低发热、减缓疼痛、僵硬和肿胀。 |
![]() ![]() Indicated PN and MES spheres were shown expressing GFP under the control of a 7 × TCF/LEF optimal promoter cassette (7 × TOP) and constitutively expressed nuclear mCherry. PN 84 and MES 1123 were treated with Wnt3a (200 ng/ml), indomethacin (Indo; 20 μM), or a control (vehicle). Scale bar, 100 μm. Bar graph, quantification of fluorescent signal of GFP (TOP-GFP) versus mCherry (PGK-H2BmCherry). The percentage of GFP- and mCherry-positive spheres was determined by FACS.
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S3168New |
cis-Resveratrolcis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) 是Resveratrol的顺式异构体。Resveratrol 是一种天然的酚类化合物,具有抗氧化、抗炎、保护心脏和抗癌的特性。Resveratrol 是 pregnane X receptor (PXR) 的抑制剂,也是 Nrf2 和 SIRT1 的激活剂,并可能诱导凋亡。Resveratrol 还可抑制多种靶标,包括 5-lipoxygenase (LOX)、cyclooxygenase (COX)、IKKβ、DNA polymerases α和δ,IC50分别为2.7 μM、<1 μM、1 μM、3.3 μM和5 μM。 |
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S2995New |
4-Hydroxyphenylpyruvic acid4-Hydroxyphenylpyruvic acid (4-HPPA) 是一种丰富的多酚结肠代谢产物,是一种有效的清除剂,可抑制 free radicals 和 cyclooxygenase-2 (COX-2) 的水平,并有助于降低结肠癌发展的风险。 |
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S3261New |
MyrislignanMyrislignan 是一种分离自Myristica fragrans Houtt的木脂素并具有抗炎活性。Myrislignan 可抑制 interleukin-6 (IL-6) 和 tumour necrosis factor-α (TNF-α)。Myrislignan 剂量依赖性地抑制LPS刺激的巨噬细胞中 inducible NO synthase (iNOS) 和 cyclooxygenase-2 (COX-2) 的表达。Myrislignan 可抑制 NF-κB 信号通路的激活。 |
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S3304New |
StylopineStylopine ((R,S)-Stylopine, Tetrahydrocoptisine) 可降低LPS刺激引起的 nitric oxide (NO)、prostaglandin E2 (PGE2)、tumor necrosis factor-alpha (TNF-alpha)、interleukin-1beta (IL-1beta) 和 IL-6 的生成,以及 cyclooxygenase-2 (COX-2) 的活性。Stylopine 是 Chelidonium majus L 的叶子的主要成分。 |
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S3255New |
PectolinarigeninPectolinarigenin 是 Cirsium chanroenicum 中的一种抗炎活性成分,是 cyclooxygenase-2 (COX-2) 和 5-lipoxygenase (5-LOX) 的双效抑制剂。 |
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S3283New |
MarmesinMarmesin (S-(+)-Marmesin, (+)-Marmesin, (S)-Marmesin) 是一种具有 COX-2 和 5-LOX 双重抑制作用的天然香豆素。 |
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S6850New |
NE 52-QQ57NE 52-QQ57 是一种 G-protein coupled receptor 4 (GPR4) 的选择性口服拮抗剂,其IC50值为0.07 μM。NE 52-QQ57 可有效地阻断GPR4介导的cAMP积累,在HEK293细胞中的IC50值为26.8 nM。NE 52-QQ57对GPR4的拮抗作用可显著地抑制AGE诱导的几种关键炎性细胞因子和信号分子表达的增加,包括 tumor necrosis factor-α (TNF-α)、interleukin (IL)-1β、IL-6、inducible nitric oxide synthase (iNOS)、nitric oxide (NO)、cyclooxygenase 2 (COX2) 和 prostaglandin E2 (PGE2)。 |
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S0821New |
PamicogrelPamicogrel (KBT3022) 是具有血小板抗聚集特性的 cyclooxygenase (COX) 的抑制剂。 |
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S2121New |
LicofeloneLicofelone (ML3000) 是COX/LOX的双重抑制剂,用于治疗骨关节炎。 |
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S0759New |
FPL 62064FPL 62064 是一种 5-lipoxygenase (5-LOX) 和 prostaglandin synthetase (cyclooxygenase, COX) 的有效双重抑制剂,对RBL-1胞质5-LOX和精囊prostaglandin synthetase的IC50值分别为3.5 μM和3.1 μM。FPL 62064 具有有效的抗炎活性。 |
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S0761New |
Desmethyl CelecoxibDesmethyl Celecoxib (compound 3b) 是一种 Celecoxib 的类似物,最佳收率为75%,是具有抗炎活性的 cyclooxygenase-2 (COX-2) 的选择性抑制剂。 |
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S0766New |
RHC 80267RHC 80267 (U-57908) 是一种有效的、具有选择性的 diacylglycerol lipase (DAGL, DAG lipase) 的抑制剂,其对 cholinesterase 活性的IC50值为4 μM。RHC 80267 可抑制 cyclooxygenase (COX) 的活性,phospholipase C (PLC) 的活性和 phosphatidylcholine (PC) 的水解作用。 |
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S6615New |
ATB 346ATB 346 是一种新的萘普生衍生物可释放硫化氢,并具有显著降低的毒性,可抑制 COX 的活性。ATB 346 是一种抗炎剂并可诱导人黑素瘤细胞的凋亡。 |
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S2595New |
FK-3311FK-3311 (COX-2 Inhibitor V)是选择性的、细胞可渗透的、口服 cyclooxygenase-2 (COX-2) 抑制剂,具有抗炎作用。FK-3311 可通过显著抑制 TxA2 来对肝热性缺血再灌注损伤起到保护作用。 |
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S6780New |
TFAPTFAP (N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide)是一种可渗透细胞的选择性 cyclooxygenase-1 (COX-1) 抑制剂,其IC50值为0.8 μM。 |
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S6686New |
SC-560SC-560 是一种高度选择性的 COX-1 抑制剂,IC50值为9 nM,而对于 COX-2 的IC50值为6.3μM 比 COX-1 高近1,000倍。 |
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S6685New |
MavacoxibMavacoxib (Trocoxil)是一种选择性的、长效的 cyclooxygenase-2 (COX-2) 抑制剂。Mavacoxib是一种新型的非甾体抗炎药(NSAID)。 |
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S2272New |
IndoprofenIndoprofen是一种非甾体类抗炎药(NSAID)和 cyclooxygenase (COX) 抑制剂。Indoprofen通过激活 PDK1/AKT pathway 来防止衰老小鼠的肌肉萎缩。Indoprofen选择性地增加 SMN2-luciferase reporter protein 和 endogenous SMN protein。 |
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S2007 |
SulindacSulindac 是一种非甾体类的COX抑制剂,有效地抑制了前列腺素的合成,用来治疗急性或者慢性炎症。 |
![]() ![]() (d) Parental and regorafenib-resistant HCT116 cells were treated with 40 μM regorafenib, 20 μM sorafenib, 1 μM UCN-01, 1 μM YM-155, 10 μM roscovitine, 15 μM sunitinib, 10 μM crizotinib, 10 nM TRAIL, 10 μM VX680, 20 μM etoposide, 20 μM temsirolimus or 120 μM sulindac sulfide for 48 h. Apoptosis was analyzed as in b. (e) Western blotting of Mcl-1 in parental and regorafenib-resistant HCT116 cells treated with indicated agents as in d for 24 h. Results in (b-d) represent the means±s.d. of three independent experiments. NS, P>0.05; *P<0.05; **P<0.01. |
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S3043 |
RofecoxibRofecoxib (MK-0966) 是一种COX-2抑制剂,IC50为18 nM。 |
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S1734 |
MeloxicamMeloxicam 是一种选择性的COX抑制剂,用于缓解疼痛以及发烧症状。 |
![]() ![]() Meloxicam (0.25 μg/ml) decreases the migration of CF41.Mg cells. Incubation with 0.25 μg/ml meloxicam for 24 and 48 h inhibited the migration of cells compared with the DMSO‑treated control cells in a wound healing assay. A total of 6 repeats were performed and results are presented as the mean ± standard deviation. Representative images of the wound healing assay and quantification if the results are presented. Scale bar, 90 μm. *P<0.05 vs. the control group.
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S4028 |
Dexamethasone Sodium PhosphateDexamethasone Sodium Phosphate是一种白介素受体抑制剂,抑制COX-2。 |
![]() ![]() Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments. |
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S3023 |
BufexamacBufexamac是一种COX抑制剂,靶点是IFN-α, EC50 为8.9 μM。 |
![]() ![]() (a) Treatment of HeLa cells with 1 mM bufexamac results in the induction of HIF1-α, as determined by immunoblotting. The known hypoxia mimetics CPX and DFX were used as positive controls; vinculin served as loading control. (b) Verification of bufexamac-specific upregulation of HIF1-α. HIF1-α protein expression was analyzed 4 h after treatment of cells with the indicated compounds. Ac, acetylated. (c) Time-course analysis of HIF1-α induction by bufexamac. The induction of HIF1-α protein was analyzed by immunoblotting. The graph shows rapid stabilization of HIF1-α upon bufexamac treatment with half-maximal intensity I1/2 of about 75 min. Error bars represent s.d. of three independent experiments. (d) HIF1-α is stabilized only at higher concentrations of bufexamac and accumulates in the nucleus. Induction of endogenous HIF1-α and its nuclear accumulation was analyzed using immunofluorescence microscopy; scale bar, 10 μm. |
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S1204 |
MelatoninMelatonin 是一种 MT receptor 激动剂激素, 用作膳食补充品。Melatonin 是一种选择性的 ATF-6 的抑制剂并可下调 COX-2。Melatonin 可增强线粒体自噬并调节凋亡和自噬的稳态。 |
![]() ![]() TUNEL staining of treated adipocytes and flow cytometry analysis of positive TUNEL cells (n=3). |
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S3017 |
AspirinAspirin (Acetylsalicylic acid) 是水杨酸类不可逆的COX1 and COX2抑制剂,常用作止痛药来缓解轻微疼痛,作为解热药减少发热,并作为一种抗炎药物。Aspirin 可诱导自噬并激发线粒体自噬。 |
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S1761 |
SuprofenSuprofen 是一种双重的COX-1/COX-2抑制剂,用作抗炎症的镇痛剂或者退热剂。 |
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S1713 |
PiroxicamPiroxicam (CP 16171) 是一种非选择性COX抑制剂,IC50为6 mM。 |
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S1328 |
EtodolacEtodolac 是COX抑制剂,IC50为53.5 nM。 |
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S1645 |
KetoprofenKetoprofen (RP-19583) 是双重 COX1/2 抑制剂,是非选择性的NSAID,作用于人重组COX-1和COX-2的 IC50分别为0.5 μM和2.33 μM。 |
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S1903 |
Diclofenac SodiumDiclofenac Sodium (GP 45840)是非选择性COX抑制剂,作用于绵羊COX-1和COX-2, IC50分别为60和220 nM。 |
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S1518 |
Ibuprofen LysineIbuprofen Lysine 是一种非甾体类抗炎药。 |
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S2047 |
LornoxicamLornoxicam (Chlortenoxicam) 是COX-1和COX-2抑制剂,IC50分别为5 nM和8 nM。 |
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S1646 |
KetorolacKetorolac是一种非选择性的COX抑制剂,作用于人类COX-1和COX-2时, IC50分别为1.23 µM和3.50 µM。 |
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S1626 |
Naproxen SodiumNaproxen Sodium (RS-3650) 是一种非选择性环氧合酶(COX)抑制剂,作用于COX-1和COX-2时,IC50分别为8.7 μM和5.2 μM。 |
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S1576 |
SulfasalazineSulfasalazine (Azulfidine, Salazopyrin, Sulphasalazine) 是一种磺胺剂,是Mesalazine的衍生物,主要用作抗炎剂。Sulfasalazine 是一种有效的、特异性的 nuclear factor kappa B (NF-κB)、TGF-β 和 COX-2 的抑制剂。Sulfasalazine 可诱导铁死亡、凋亡和自噬。 |
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S2903 |
LumiracoxibLumiracoxib (COX-189)是一种新型,选择性的COX-2抑制剂,Ki为0.06 μM;对COX1的Ki值为3 μM。 |
![]() ![]() (A) Western blot analysis of MITF expression in MelIM. One representative experiment out of two is shown. (B) Proliferation of MelIM cells under diclofenac or lumiracoxib (0.1 mM) for 3 vs. 30 days. Results are given as percentage of untreated controls.
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S2531 |
AsaraldehydeAsaraldehyde (Asaronaldehyde)是一种天然的COX-2抑制剂,比作用于COX-1选择性高17倍。 |
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S1960 |
PranoprofenPranoprofen (Pyranoprofen) 是PGE2抑制剂,IC50为7.5 μM。 |
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S2410 |
PaeoniflorinPaeoniflorin 是一种从Paeonia albiflora Pall根部提取的中草药成分。Paeoniflorin 可降低 COX-2 表达。Paeoniflorin 可通过mTOR依赖的通路抑制 HIF-1α 来减轻肝纤维化。 |
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S3008 |
ZaltoprofenZaltoprofen是COX-1和COX-2抑制剂,用于治疗关节炎。 |
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S2602 |
AcemetacinAcemetacin (K-708) 是一种非甾体类抗炎药,是吲哚美辛的乙醇酸酯,是一种环加氧酶抑制剂。 |
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S1959 |
Tolfenamic AcidTolfenamic Acid是一种COX-2抑制剂,IC50为0.2 μM。 |
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S4049 |
ValdecoxibValdecoxib是一种强有效和选择性的COX-2抑制剂,IC50为5nM. |
![]() ![]() (B) HeLa and SACC-83 cells were treated with radiation, valdecoxib, or both radiation and valdecoxib. Cells were lysed or extracted for membrane proteins and then subjected to Western blot. |
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S2577 |
PhenacetinPhenacetin (Acetophenetidin)是一种非阿片类镇痛剂,没有抗炎特性。 |
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S2040 |
NimesulideNimesulide是一种选择性COX-2抑制剂,IC50为26 μM。 |
![]() ![]() Nimesulide has no effect on KSHV lytic replication in BCBL-1 cells. The cells induced with TPA for 3 h were treated with the test compounds for 72 h. Then, the effect of nimesulide on cell viability (C) and the number of DNA copies (D) were measured as described in the Methods. CDV (20 µM) is a positive control for inhibiting viral DNA replication. Data were normalized as the fold change compared with the no-TPA induced control. The results are presented as the mean values with standard deviations (n = 3). |
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S4149 |
Amfenac Sodium MonohydrateAmfenac Sodium Monohydrate是一种非甾体类镇痛消炎药。对COX1和COX2的IC50分别为250 nM和150 nM。 |
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S4248 |
Bromfenac SodiumBromfenac Sodium (AHR 10282R)是一种非甾体类抗炎药(NSAID),具有抗炎活性,通过抑制环氧合酶1和2可阻断前列腺素的合成。 |
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S4051 |
NabumetoneNabumetone (BRL-14777) 是一种非甾类抗炎症药物,它的活性代谢物抑制COX。 |
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S3018 |
Niflumic acidNiflumic acid是环氧合酶-2 (COX-2)抑制剂,用于治疗关节和肌肉疼痛。 |
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S3173 |
AntipyrineAntipyrine (Phenazone) 是一种镇痛剂和退热剂,选择性COX3抑制剂。 |
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S9190 |
Oroxin BOroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels are downregulated, while PTEN is upregulated after Oroxin B treatment. |
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S3200 |
TriflusalTriflusal (UR1501)是一种抗血栓药剂,通过乙酰化环氧化酶-1来不可逆的抑制血小板中血栓素-B2的产生。 |
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S4011 |
AmpiroxicamAmpiroxicam (CP 65703)是一种非选择性的cyclooxygenase(环氧合酶)抑制剂,作为消炎药。 |
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S9208 |
Ginsenoside Rb3Ginsenoside Rb3 是从人参中提取的天然产物,在心血管疾病包括心肌的缺血/再灌注(I/R)损伤中起着重要作用。在人肾293T细胞中检测了Ginsenoside Rb3(0.1-10 μM)对肿瘤坏死因子TNF-α诱导的 nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) 荧光素酶报告基因的抑制作用,IC50值为8.2 μM。在用10 ng/mL TNF-α处理后的HepG2细胞中,Ginsenoside Rb3 还以剂量依赖性的方式抑制 cyclooxygenase-2 (COX-2) 和 inducible nitric oxide synthase (iNOS) 信使mRNA的诱导诱导表达。 |
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S5177 |
NaproxenNaproxen is an anti-inflammatory agent with analgesic and antipyretic properties. It is a nonselective inhibitor of COX-1 and COX-2. |
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S5418 |
Parecoxib SodiumParecoxib Sodium (SC-69124) is a water-soluble, injectable sodium salt form of parecoxib, which is a potent and selective inhibitor of cyclo-oxygenase-2 (COX2). |
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S3969 |
Veratric acidVeratric acid (3,4-Dimethoxybenzoic acid)是一种来自植物和水果的简单苯甲酸,具有抗氧化,抗发炎和降血压的作用。Veratric acid 可降低UVB照射后上调的 COX-2 的表达以及 PGE2、IL-6 的水平。 |
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S9236 |
α-Cyperoneα-Cyperone (alpha-cyperone) 是香附子Cyperus rotundus的主要活性成分,表现出了如抗毒力、抗原毒性和抗菌活性等生物活性。α-Cyperone (alpha-cyperone) 与COX-2、IL-6、Nck-2、Cdc42 和 Rac1 的表达下调有关。 |
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S3816 |
DehydroevodiamineDehydroevodiamine (DHED), a constituent of Evodia rutaecarpa, has various biological effects such as hypotensive, negative chronotropic, ion channel depressant, inhibition of nitric oxide production and cerebral blood flow enhancing activities. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells. |
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S8433 |
NS-398 (NS398)NS-398 (N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide) 是一种选择性的COX-2抑制剂,对人源重组的COX-1和COX-2的IC50分别为75 μM和1.77μM。 |
![]() ![]() (C)Percentage of TUNEL-positive cell in B were calculated. Data are mean ± SEM; ** P < 0.01 versus the Sham group; # P < 0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group. (D-G) ELISA of cytokines IL-1α (D), IL-1β (E), IL-6 (F), and TNF-α (G) in tSCI rats with or without NS-398 treatment. Data are mean ± SEM; * P < 0.05 or ** P < 0.01 versus the Sham group; # P <0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group. (H) The mean CBS score in tSCI rats was improved by NS-398 treatment. Data are mean ± SEM; ** P < 0.05 versus the Sham group; # P < 0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group.
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S4032 |
Bismuth SubsalicylateBismuth Subsalicylate 是Pepto-Bismol的有效成分,可以抑制前列腺素G/H合成酶1/2。 |
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S5698 |
Ketorolac tromethamine saltKetorolac tromethamine是一种合成的吡呤环羧酸衍生物,具有消炎、止痛和退热活性。它是非选择性的COX抑制剂,对COX-1和COX-2的IC50值都是20 nM。 |
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S4628 |
(+/-)-SulfinpyrazoneSulfinpyrazone (G-28315, NSC 75925)是研究得最多的血小板COX抑制剂之一,还是一种能在肾脏近端小管中,竞争性抑制尿酸重吸收的尿酸排泄剂。 |
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S4136 |
CarprofenCarprofen 抑制犬科COX2,IC50为30 nM。 |
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S3063 |
Diclofenac DiethylamineDiclofenac Diethylamine是一种非类固醇消炎药,用于减轻炎症和某些状况下的止痛药。Diclofenac通过抑制COX1和COX2来抑制前列腺素合成,发挥其功能。 |
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S3974 |
(+)-Catechin hydrateCatechins are a plant derived polyphenolic anti-oxidants with phytotoxic properties. (+)-Catechin hydrate is a frequent component of traditional herbal remedies, such as Uncaria rhynchophylla. |
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S4656 |
ParecoxibParecoxib (SC-69124, Valus-P, Vorth-P) 是选择性COX2的抑制剂。 |
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S4609 |
DiflunisalDiflunisal (Dolobid, Dolobis, Flovacil, Fluniget)是水杨酸的二氟苯基衍生物,是非类固醇的消炎药。具有退热、止痛和消炎特性。它是环氧酶抑制剂。 |
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S4176 |
TrometamolTrometamol是一种质子受体,用于治疗酸血症。它能抑制COX1和COX2,因而抑制花生四烯酸向炎性前列腺素的转变。 |
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S5520 |
PhenidonePhenidone (1-phenyl-3-pyrazolidinone), a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), is an organic compound that is primarily used as a photographic developer. |
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S9029 |
Prim-o-glucosylcimifuginPrim-O-glucosylcimifugin (Cimifugin beta-D-glucopyranoside, Cimifugin 7-glucoside) 是防风(Radix Saposhnikovia)中的主要成分,长期以来一直应用于传统中医药中治疗发热、风湿和癌症,它表现出潜在的抗癌活性。在LPS激活的 RAW 264.7 巨噬细胞,Prim-O-glucosylcimifugin 可以浓度依赖性的方式下调 NO synthase (iNOS) 和 cyclooxygenase 2 (COX-2) 的mRNA和蛋白质表达。 |
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S3931 |
Ginsenoside RdGinsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively. |
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S5019 |
IndobufenIndobufen (Ibustrin, K 3920) 是一种可逆的 platelet aggregation 的抑制剂。 Indobufen 是 platelet cyclooxygenase (Cox) 活性的抑制剂,并能抑制凝血恶烷的合成。 |
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S4078 |
Mefenamic AcidMefenamic Acid (CI 473, CN-35355) 是一种竞争性COX-1和COX-2抑制剂。 |
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S4651 |
EtoricoxibEtoricoxib (Arcoxia, MK-663, MK-0663, Tauxib, Algix, Nucoxia)是一种新型的COX-2选择性抑制剂,具有抗炎、退热、止痛和潜在的抗肿瘤活性。 |
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S9386 |
Polygalacic acidPolygalacic acid 是从远志属植物(Polygala paenea L.)分离出的三萜类四羟酸。Polygalacic acid (0-100μM; 24h) 可以显著降低 MMP-3、MMP-9、MMP-13 和 COX-2 的mRNA表达,这些因子的表达由IL-1β诱导可显著增加,并呈现出剂量依赖性。 |
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S4686 |
Vitamin EVitamin E (D-alpha-Tocopherol) 是一种脂溶性的维生素,具有有效的抗氧化特性。它是有效的过氧化氢自由基清除剂并在很多组织中,非竞争性地抑制环氧酶活性。同时通过抑制VEGF基因转录,抑制血管生成和肿瘤休眠。 |
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S6073 |
Diclofenac acidDiclofenac acid是一种非类固醇的消炎药,具有止痛、消炎和退热活性,在治疗多种急性和慢性疼痛、炎症反应中有效。它能抑制cyclooxygenase-1 (COX-1)和cyclooxygenase-2 (COX-2),具有相近的效力。 |
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S4765 |
SyringaldehydeSyringaldehyde (Syringic aldehyde) is an organic compound that occurs naturally in trace amounts. It possesses worthy bioactive properties and is, therefore, used in pharmaceuticals, food, cosmetics, textiles, pulp and paper industries, and even in biological control applications. |
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S5010 |
Indometacin SodiumIndomethacin Sodium (Indometacin Sodium) is the sodium salt of indomethacin, which is a non-selective, reversible, and competitive inhibitor of cyclooxygenases 1 and 2 with anti-inflammatory, analgesic-antipyretic and tocolytic effects. |
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S4230 |
OxaprozinOxaprozin 是一种非麻醉性,非甾体类抗炎药(NSAID),用于缓解与骨关节炎和类风湿关节炎相关的炎症,肿胀,僵硬,关节疼痛。 |
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S5595 |
3-Carene3-Carene (Carene, Delta-3-Carene)是在从松树中提取的精油中的双环单萜。 3-Carene对 COX-2 过表达和LPS诱导的Raw264.7巨噬细胞迁移具有强大的药理作用。3-Carene被证明可显着刺激 alkaline phosphatase 的活性和表达 ,是成骨细胞分化的早期标志。 |
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S2349 |
RutaecarpineRutaecarpine (Rutecarpine) 是从 Evodia rutaecarpa和相关草药中分离的indolopyridoquinazolinone生物碱。是一种新型的COX2抑制剂。 |
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S4360 |
Tolmetin SodiumTolmetin is a non-steroidal anti-inflammatory drug of the arylalkanoic acids. |
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S2351 |
SalicinSalicin (Salicoside, Salicine)是一种醇-β-糖苷,含有D-葡萄糖。是柳树皮产生的一种抗炎剂。它是一种天然的、非选择性的COX1和COX2抑制剂。 |
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S4526 |
FenbufenFenbufen (Lederfen, CL-82204) 是一种具有口服活性的苯基链烷衍生物(phenylalkanoic derivative),它具有抗炎、止痛、解热的活性,是一种非固醇类的消炎药。 |
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S3899 |
HederageninHederagenin (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo. Hederagenin inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB. |
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S5551 |
6-Paradol6-Paradol is a minor constituent of ginger, mainly formed from 6-gingerol via 6-shogaol, and exhibits a variety of biological activities including anti-cancer, anti-inflammatory, and anti-oxidative activities. |
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S9502 |
Madecassic acidMadecassic acid (Brahmic acid) 是最早从积雪草中分离的天然三萜,具有多种消炎和抗糖尿病作用,阻断巨噬细胞中的 NF-κB 活化并导致 iNOS、COX-2、TNF-alpha、IL-1beta 和 IL-6 抑制。 |
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S4539 |
Salicylic acidSalicylic acid (2-Hydroxybenzoic acid)是一种水杨酸,植物中的天然化合物,是乙烯生物合成和环氧酶活性的抑制剂。 |
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S9149 |
BenzoylpaeoniflorinBenzoylpaeoniflorin, a natural product isolated from Chinese paeony root, could inhibit COX-1 and COX-2 in vitro. |
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S6457 |
Flurbiprofen AxetilFlurbiprofen Axetil是一种常用的消炎药,可非特异性地抑制环氧酶COX。 |
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S4509 |
4-Aminoantipyrine4-Aminoantipyrine(Ampyrone, NSC 60242, Metapirazone, Solnapyrin-A, Solvapyrin-A, Minoazophene, Aminoazophene) 是aminopyrine的代谢产物,具有镇痛、消炎退热的效果。Ampyrone刺激肝微粒体,用来测定胞外液。 |
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S3872 |
GuaiacolGuaiacol (O-methoxyphenol, 2-hydroxyanisole, O-methylcatechol) is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. It is a precursor to various flavorants, such as eugenoland vanillin. Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity. |
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S5309 |
Propyphenazone (4-Isopropylantipyrine)Propyphenazone(4-Isopropylantipyrine, Isopropyrine) 是一种止痛退热试剂,一种选择性的 cyclooxygenase-2 抑制剂,具有消炎活性。 |
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S7889 |
XanthohumolXanthohumol,来自啤酒花的一种异戊烯化查耳酮,抑制COX-1和COX-2活性,并表现出化学预防作用。Xanthohumol 可抑制 diacylglycerol acyltransferase 1 (DGAT1) 和 DGAT2,对应的IC50值均为40 μM。Xanthohumol 也是一种有效的针对一系列DNA和RNA病毒的抗病毒药剂。Xanthohumol 在肿瘤细胞中可诱导生长阻滞和凋亡。Phase 1。 |
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S2108 |
Flunixin MegluminFlunixin Meglumin是一种有效的环氧化酶抑制剂,用作镇痛剂,具有抗炎和退热的活性。 |
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S5711 |
DeracoxibDeracoxib (SC-046) is a COX-2 inhibitor with >48-fold selectivity over COX-1. It also exhibits inhibitory activity against phosphodiesterase (Ki = 3.6 μM against human PDE4D3). |
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S3925 |
(-)-Epicatechin gallate(-)-Epicatechin gallate (ECG) 是一种 cyclooxygenase-1 (COX-1) 的抑制剂,IC50值为7.5 μM。 |
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S4295 |
Meclofenamate SodiumMeclofenamate Sodium 是一种双 COX-1/COX-2 抑制剂,其 IC50 分别为40 nM 和 50 nM,用于治疗关节、肌肉疼痛,关节炎以及痛经。Meclofenamate Sodium 是一种非选择性 gap-junction 的阻断剂和高选择性的 fat mass and obesity-associated (FTO) enzyme 抑制剂。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S1261 |
CelecoxibCelecoxib (SC 58635) 是一种选择性COX-2抑制剂,在Sf9细胞中IC50为40 nM。 |
![]() ![]() Reduced hepatic lipid contents and alleviated liver injury in EC-AMPK mice treated with selective COX-2 inhibitors. Wild-type and EC-AMPK mice given a high fat diet were treated with vehicle, celecoxib or nimesulide for a period of 4 weeks. At the end of treatment, parameters including body weight and circulating glucose (A), serum triglyceride and cholesterol levels (B were measured and presented as percentage comparisons against those from vehicle-treated wild-type mice. *P < 0.05 versus wild-type mice treated with vehicle; #P < 0.05 versus EC-AMPK mice treated with vehicle, n = 3-5. |
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S1396 |
ResveratrolResveratrol具有广泛靶点,包括环氧酶(如COX, IC50=1.1 μM)、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素,具有抗癌,抗炎,降血糖和其他有益心血管的作用。Resveratrol可诱导线粒体自噬、细胞自噬和自噬依赖性的凋亡。 |
![]() ![]() Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours. |
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S1255 |
NepafenacNepafenac (AHR 9434, AL 6515) 是一种非甾体抗炎药剂。 |
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S1638 |
IbuprofenIbuprofen 是一种抗炎类抑制剂,作用于COX-1和COX-2,IC50分别为13 μM和370 μM。 |
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S1723 |
IndomethacinIndomethacin是一种非选择性的COX1和COX2的抑制剂,IC50分别为0.1 μg/mL和5 μg/mL。常用于降低发热、减缓疼痛、僵硬和肿胀。 |
![]() ![]() Indicated PN and MES spheres were shown expressing GFP under the control of a 7 × TCF/LEF optimal promoter cassette (7 × TOP) and constitutively expressed nuclear mCherry. PN 84 and MES 1123 were treated with Wnt3a (200 ng/ml), indomethacin (Indo; 20 μM), or a control (vehicle). Scale bar, 100 μm. Bar graph, quantification of fluorescent signal of GFP (TOP-GFP) versus mCherry (PGK-H2BmCherry). The percentage of GFP- and mCherry-positive spheres was determined by FACS.
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S3168New |
cis-Resveratrolcis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) 是Resveratrol的顺式异构体。Resveratrol 是一种天然的酚类化合物,具有抗氧化、抗炎、保护心脏和抗癌的特性。Resveratrol 是 pregnane X receptor (PXR) 的抑制剂,也是 Nrf2 和 SIRT1 的激活剂,并可能诱导凋亡。Resveratrol 还可抑制多种靶标,包括 5-lipoxygenase (LOX)、cyclooxygenase (COX)、IKKβ、DNA polymerases α和δ,IC50分别为2.7 μM、<1 μM、1 μM、3.3 μM和5 μM。 |
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S2995New |
4-Hydroxyphenylpyruvic acid4-Hydroxyphenylpyruvic acid (4-HPPA) 是一种丰富的多酚结肠代谢产物,是一种有效的清除剂,可抑制 free radicals 和 cyclooxygenase-2 (COX-2) 的水平,并有助于降低结肠癌发展的风险。 |
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S3261New |
MyrislignanMyrislignan 是一种分离自Myristica fragrans Houtt的木脂素并具有抗炎活性。Myrislignan 可抑制 interleukin-6 (IL-6) 和 tumour necrosis factor-α (TNF-α)。Myrislignan 剂量依赖性地抑制LPS刺激的巨噬细胞中 inducible NO synthase (iNOS) 和 cyclooxygenase-2 (COX-2) 的表达。Myrislignan 可抑制 NF-κB 信号通路的激活。 |
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S3304New |
StylopineStylopine ((R,S)-Stylopine, Tetrahydrocoptisine) 可降低LPS刺激引起的 nitric oxide (NO)、prostaglandin E2 (PGE2)、tumor necrosis factor-alpha (TNF-alpha)、interleukin-1beta (IL-1beta) 和 IL-6 的生成,以及 cyclooxygenase-2 (COX-2) 的活性。Stylopine 是 Chelidonium majus L 的叶子的主要成分。 |
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S3255New |
PectolinarigeninPectolinarigenin 是 Cirsium chanroenicum 中的一种抗炎活性成分,是 cyclooxygenase-2 (COX-2) 和 5-lipoxygenase (5-LOX) 的双效抑制剂。 |
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S3283New |
MarmesinMarmesin (S-(+)-Marmesin, (+)-Marmesin, (S)-Marmesin) 是一种具有 COX-2 和 5-LOX 双重抑制作用的天然香豆素。 |
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S6850New |
NE 52-QQ57NE 52-QQ57 是一种 G-protein coupled receptor 4 (GPR4) 的选择性口服拮抗剂,其IC50值为0.07 μM。NE 52-QQ57 可有效地阻断GPR4介导的cAMP积累,在HEK293细胞中的IC50值为26.8 nM。NE 52-QQ57对GPR4的拮抗作用可显著地抑制AGE诱导的几种关键炎性细胞因子和信号分子表达的增加,包括 tumor necrosis factor-α (TNF-α)、interleukin (IL)-1β、IL-6、inducible nitric oxide synthase (iNOS)、nitric oxide (NO)、cyclooxygenase 2 (COX2) 和 prostaglandin E2 (PGE2)。 |
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S0821New |
PamicogrelPamicogrel (KBT3022) 是具有血小板抗聚集特性的 cyclooxygenase (COX) 的抑制剂。 |
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S2121New |
LicofeloneLicofelone (ML3000) 是COX/LOX的双重抑制剂,用于治疗骨关节炎。 |
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S0759New |
FPL 62064FPL 62064 是一种 5-lipoxygenase (5-LOX) 和 prostaglandin synthetase (cyclooxygenase, COX) 的有效双重抑制剂,对RBL-1胞质5-LOX和精囊prostaglandin synthetase的IC50值分别为3.5 μM和3.1 μM。FPL 62064 具有有效的抗炎活性。 |
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S0761New |
Desmethyl CelecoxibDesmethyl Celecoxib (compound 3b) 是一种 Celecoxib 的类似物,最佳收率为75%,是具有抗炎活性的 cyclooxygenase-2 (COX-2) 的选择性抑制剂。 |
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S0766New |
RHC 80267RHC 80267 (U-57908) 是一种有效的、具有选择性的 diacylglycerol lipase (DAGL, DAG lipase) 的抑制剂,其对 cholinesterase 活性的IC50值为4 μM。RHC 80267 可抑制 cyclooxygenase (COX) 的活性,phospholipase C (PLC) 的活性和 phosphatidylcholine (PC) 的水解作用。 |
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S6615New |
ATB 346ATB 346 是一种新的萘普生衍生物可释放硫化氢,并具有显著降低的毒性,可抑制 COX 的活性。ATB 346 是一种抗炎剂并可诱导人黑素瘤细胞的凋亡。 |
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S2595New |
FK-3311FK-3311 (COX-2 Inhibitor V)是选择性的、细胞可渗透的、口服 cyclooxygenase-2 (COX-2) 抑制剂,具有抗炎作用。FK-3311 可通过显著抑制 TxA2 来对肝热性缺血再灌注损伤起到保护作用。 |
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S6780New |
TFAPTFAP (N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide)是一种可渗透细胞的选择性 cyclooxygenase-1 (COX-1) 抑制剂,其IC50值为0.8 μM。 |
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S6686New |
SC-560SC-560 是一种高度选择性的 COX-1 抑制剂,IC50值为9 nM,而对于 COX-2 的IC50值为6.3μM 比 COX-1 高近1,000倍。 |
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S6685New |
MavacoxibMavacoxib (Trocoxil)是一种选择性的、长效的 cyclooxygenase-2 (COX-2) 抑制剂。Mavacoxib是一种新型的非甾体抗炎药(NSAID)。 |
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S2272New |
IndoprofenIndoprofen是一种非甾体类抗炎药(NSAID)和 cyclooxygenase (COX) 抑制剂。Indoprofen通过激活 PDK1/AKT pathway 来防止衰老小鼠的肌肉萎缩。Indoprofen选择性地增加 SMN2-luciferase reporter protein 和 endogenous SMN protein。 |
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S2007 |
SulindacSulindac 是一种非甾体类的COX抑制剂,有效地抑制了前列腺素的合成,用来治疗急性或者慢性炎症。 |
![]() ![]() (d) Parental and regorafenib-resistant HCT116 cells were treated with 40 μM regorafenib, 20 μM sorafenib, 1 μM UCN-01, 1 μM YM-155, 10 μM roscovitine, 15 μM sunitinib, 10 μM crizotinib, 10 nM TRAIL, 10 μM VX680, 20 μM etoposide, 20 μM temsirolimus or 120 μM sulindac sulfide for 48 h. Apoptosis was analyzed as in b. (e) Western blotting of Mcl-1 in parental and regorafenib-resistant HCT116 cells treated with indicated agents as in d for 24 h. Results in (b-d) represent the means±s.d. of three independent experiments. NS, P>0.05; *P<0.05; **P<0.01. |
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S3043 |
RofecoxibRofecoxib (MK-0966) 是一种COX-2抑制剂,IC50为18 nM。 |
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S1734 |
MeloxicamMeloxicam 是一种选择性的COX抑制剂,用于缓解疼痛以及发烧症状。 |
![]() ![]() Meloxicam (0.25 μg/ml) decreases the migration of CF41.Mg cells. Incubation with 0.25 μg/ml meloxicam for 24 and 48 h inhibited the migration of cells compared with the DMSO‑treated control cells in a wound healing assay. A total of 6 repeats were performed and results are presented as the mean ± standard deviation. Representative images of the wound healing assay and quantification if the results are presented. Scale bar, 90 μm. *P<0.05 vs. the control group.
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S4028 |
Dexamethasone Sodium PhosphateDexamethasone Sodium Phosphate是一种白介素受体抑制剂,抑制COX-2。 |
![]() ![]() Dexamethasone and largazole cooperate to suppress invasion and to restore E-cadherin localization to the cell peripher y. ( a) Phase contrast micrographs showing morphological changes in MDA-MB-231 cells induced by E-cadherin expression combined with 100 nM dexamethasone and 10 nM largazole treatments. Insets show the cells at higher magnification. (b ) Fluorescence (E-Cad-GFP) or immunofluorescence microscopy (g -catenin (g-Cat.)) of 231/E-Cad-GFP cells treated for 72 h with vehicle (Control), 100 n M dexamethasone, 10 nM largazole or 100 nM dexamethasone + 10 nM largazole (Dex. + Larg.). (c ) Invasion assays were per formed with the indicated cell lines treated for 72 h with or without 100 nM dexamethasone + 10 nM largazole using modified Boyden chambers impregnated with matrigel. The results are presented as the average number of cells that invaded through the membrane per field s.d. of five randomly chosen fields, and are representative of three independently per formed experiments. |
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S3023 |
BufexamacBufexamac是一种COX抑制剂,靶点是IFN-α, EC50 为8.9 μM。 |
![]() ![]() (a) Treatment of HeLa cells with 1 mM bufexamac results in the induction of HIF1-α, as determined by immunoblotting. The known hypoxia mimetics CPX and DFX were used as positive controls; vinculin served as loading control. (b) Verification of bufexamac-specific upregulation of HIF1-α. HIF1-α protein expression was analyzed 4 h after treatment of cells with the indicated compounds. Ac, acetylated. (c) Time-course analysis of HIF1-α induction by bufexamac. The induction of HIF1-α protein was analyzed by immunoblotting. The graph shows rapid stabilization of HIF1-α upon bufexamac treatment with half-maximal intensity I1/2 of about 75 min. Error bars represent s.d. of three independent experiments. (d) HIF1-α is stabilized only at higher concentrations of bufexamac and accumulates in the nucleus. Induction of endogenous HIF1-α and its nuclear accumulation was analyzed using immunofluorescence microscopy; scale bar, 10 μm. |
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S1204 |
MelatoninMelatonin 是一种 MT receptor 激动剂激素, 用作膳食补充品。Melatonin 是一种选择性的 ATF-6 的抑制剂并可下调 COX-2。Melatonin 可增强线粒体自噬并调节凋亡和自噬的稳态。 |
![]() ![]() TUNEL staining of treated adipocytes and flow cytometry analysis of positive TUNEL cells (n=3). |
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S3017 |
AspirinAspirin (Acetylsalicylic acid) 是水杨酸类不可逆的COX1 and COX2抑制剂,常用作止痛药来缓解轻微疼痛,作为解热药减少发热,并作为一种抗炎药物。Aspirin 可诱导自噬并激发线粒体自噬。 |
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S1761 |
SuprofenSuprofen 是一种双重的COX-1/COX-2抑制剂,用作抗炎症的镇痛剂或者退热剂。 |
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S1713 |
PiroxicamPiroxicam (CP 16171) 是一种非选择性COX抑制剂,IC50为6 mM。 |
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S1328 |
EtodolacEtodolac 是COX抑制剂,IC50为53.5 nM。 |
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S1645 |
KetoprofenKetoprofen (RP-19583) 是双重 COX1/2 抑制剂,是非选择性的NSAID,作用于人重组COX-1和COX-2的 IC50分别为0.5 μM和2.33 μM。 |
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S1903 |
Diclofenac SodiumDiclofenac Sodium (GP 45840)是非选择性COX抑制剂,作用于绵羊COX-1和COX-2, IC50分别为60和220 nM。 |
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S1518 |
Ibuprofen LysineIbuprofen Lysine 是一种非甾体类抗炎药。 |
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S2047 |
LornoxicamLornoxicam (Chlortenoxicam) 是COX-1和COX-2抑制剂,IC50分别为5 nM和8 nM。 |
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S1646 |
KetorolacKetorolac是一种非选择性的COX抑制剂,作用于人类COX-1和COX-2时, IC50分别为1.23 µM和3.50 µM。 |
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S1626 |
Naproxen SodiumNaproxen Sodium (RS-3650) 是一种非选择性环氧合酶(COX)抑制剂,作用于COX-1和COX-2时,IC50分别为8.7 μM和5.2 μM。 |
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S1576 |
SulfasalazineSulfasalazine (Azulfidine, Salazopyrin, Sulphasalazine) 是一种磺胺剂,是Mesalazine的衍生物,主要用作抗炎剂。Sulfasalazine 是一种有效的、特异性的 nuclear factor kappa B (NF-κB)、TGF-β 和 COX-2 的抑制剂。Sulfasalazine 可诱导铁死亡、凋亡和自噬。 |
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S2903 |
LumiracoxibLumiracoxib (COX-189)是一种新型,选择性的COX-2抑制剂,Ki为0.06 μM;对COX1的Ki值为3 μM。 |
![]() ![]() (A) Western blot analysis of MITF expression in MelIM. One representative experiment out of two is shown. (B) Proliferation of MelIM cells under diclofenac or lumiracoxib (0.1 mM) for 3 vs. 30 days. Results are given as percentage of untreated controls.
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S2531 |
AsaraldehydeAsaraldehyde (Asaronaldehyde)是一种天然的COX-2抑制剂,比作用于COX-1选择性高17倍。 |
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S1960 |
PranoprofenPranoprofen (Pyranoprofen) 是PGE2抑制剂,IC50为7.5 μM。 |
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S2410 |
PaeoniflorinPaeoniflorin 是一种从Paeonia albiflora Pall根部提取的中草药成分。Paeoniflorin 可降低 COX-2 表达。Paeoniflorin 可通过mTOR依赖的通路抑制 HIF-1α 来减轻肝纤维化。 |
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S3008 |
ZaltoprofenZaltoprofen是COX-1和COX-2抑制剂,用于治疗关节炎。 |
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S2602 |
AcemetacinAcemetacin (K-708) 是一种非甾体类抗炎药,是吲哚美辛的乙醇酸酯,是一种环加氧酶抑制剂。 |
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S1959 |
Tolfenamic AcidTolfenamic Acid是一种COX-2抑制剂,IC50为0.2 μM。 |
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S4049 |
ValdecoxibValdecoxib是一种强有效和选择性的COX-2抑制剂,IC50为5nM. |
![]() ![]() (B) HeLa and SACC-83 cells were treated with radiation, valdecoxib, or both radiation and valdecoxib. Cells were lysed or extracted for membrane proteins and then subjected to Western blot. |
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S2577 |
PhenacetinPhenacetin (Acetophenetidin)是一种非阿片类镇痛剂,没有抗炎特性。 |
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S2040 |
NimesulideNimesulide是一种选择性COX-2抑制剂,IC50为26 μM。 |
![]() ![]() Nimesulide has no effect on KSHV lytic replication in BCBL-1 cells. The cells induced with TPA for 3 h were treated with the test compounds for 72 h. Then, the effect of nimesulide on cell viability (C) and the number of DNA copies (D) were measured as described in the Methods. CDV (20 µM) is a positive control for inhibiting viral DNA replication. Data were normalized as the fold change compared with the no-TPA induced control. The results are presented as the mean values with standard deviations (n = 3). |
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S4149 |
Amfenac Sodium MonohydrateAmfenac Sodium Monohydrate是一种非甾体类镇痛消炎药。对COX1和COX2的IC50分别为250 nM和150 nM。 |
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S4248 |
Bromfenac SodiumBromfenac Sodium (AHR 10282R)是一种非甾体类抗炎药(NSAID),具有抗炎活性,通过抑制环氧合酶1和2可阻断前列腺素的合成。 |
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S4051 |
NabumetoneNabumetone (BRL-14777) 是一种非甾类抗炎症药物,它的活性代谢物抑制COX。 |
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S3018 |
Niflumic acidNiflumic acid是环氧合酶-2 (COX-2)抑制剂,用于治疗关节和肌肉疼痛。 |
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S3173 |
AntipyrineAntipyrine (Phenazone) 是一种镇痛剂和退热剂,选择性COX3抑制剂。 |
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S9190 |
Oroxin BOroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels are downregulated, while PTEN is upregulated after Oroxin B treatment. |
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S3200 |
TriflusalTriflusal (UR1501)是一种抗血栓药剂,通过乙酰化环氧化酶-1来不可逆的抑制血小板中血栓素-B2的产生。 |
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S4011 |
AmpiroxicamAmpiroxicam (CP 65703)是一种非选择性的cyclooxygenase(环氧合酶)抑制剂,作为消炎药。 |
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S9208 |
Ginsenoside Rb3Ginsenoside Rb3 是从人参中提取的天然产物,在心血管疾病包括心肌的缺血/再灌注(I/R)损伤中起着重要作用。在人肾293T细胞中检测了Ginsenoside Rb3(0.1-10 μM)对肿瘤坏死因子TNF-α诱导的 nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) 荧光素酶报告基因的抑制作用,IC50值为8.2 μM。在用10 ng/mL TNF-α处理后的HepG2细胞中,Ginsenoside Rb3 还以剂量依赖性的方式抑制 cyclooxygenase-2 (COX-2) 和 inducible nitric oxide synthase (iNOS) 信使mRNA的诱导诱导表达。 |
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S5177 |
NaproxenNaproxen is an anti-inflammatory agent with analgesic and antipyretic properties. It is a nonselective inhibitor of COX-1 and COX-2. |
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S5418 |
Parecoxib SodiumParecoxib Sodium (SC-69124) is a water-soluble, injectable sodium salt form of parecoxib, which is a potent and selective inhibitor of cyclo-oxygenase-2 (COX2). |
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S3969 |
Veratric acidVeratric acid (3,4-Dimethoxybenzoic acid)是一种来自植物和水果的简单苯甲酸,具有抗氧化,抗发炎和降血压的作用。Veratric acid 可降低UVB照射后上调的 COX-2 的表达以及 PGE2、IL-6 的水平。 |
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S9236 |
α-Cyperoneα-Cyperone (alpha-cyperone) 是香附子Cyperus rotundus的主要活性成分,表现出了如抗毒力、抗原毒性和抗菌活性等生物活性。α-Cyperone (alpha-cyperone) 与COX-2、IL-6、Nck-2、Cdc42 和 Rac1 的表达下调有关。 |
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S3816 |
DehydroevodiamineDehydroevodiamine (DHED), a constituent of Evodia rutaecarpa, has various biological effects such as hypotensive, negative chronotropic, ion channel depressant, inhibition of nitric oxide production and cerebral blood flow enhancing activities. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells. |
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S8433 |
NS-398 (NS398)NS-398 (N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide) 是一种选择性的COX-2抑制剂,对人源重组的COX-1和COX-2的IC50分别为75 μM和1.77μM。 |
![]() ![]() (C)Percentage of TUNEL-positive cell in B were calculated. Data are mean ± SEM; ** P < 0.01 versus the Sham group; # P < 0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group. (D-G) ELISA of cytokines IL-1α (D), IL-1β (E), IL-6 (F), and TNF-α (G) in tSCI rats with or without NS-398 treatment. Data are mean ± SEM; * P < 0.05 or ** P < 0.01 versus the Sham group; # P <0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group. (H) The mean CBS score in tSCI rats was improved by NS-398 treatment. Data are mean ± SEM; ** P < 0.05 versus the Sham group; # P < 0.05 versus the Vehicle group; unpaired two-tailed Student’s t-test. n = 5 per group.
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S4032 |
Bismuth SubsalicylateBismuth Subsalicylate 是Pepto-Bismol的有效成分,可以抑制前列腺素G/H合成酶1/2。 |
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S5698 |
Ketorolac tromethamine saltKetorolac tromethamine是一种合成的吡呤环羧酸衍生物,具有消炎、止痛和退热活性。它是非选择性的COX抑制剂,对COX-1和COX-2的IC50值都是20 nM。 |
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S4628 |
(+/-)-SulfinpyrazoneSulfinpyrazone (G-28315, NSC 75925)是研究得最多的血小板COX抑制剂之一,还是一种能在肾脏近端小管中,竞争性抑制尿酸重吸收的尿酸排泄剂。 |
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S4136 |
CarprofenCarprofen 抑制犬科COX2,IC50为30 nM。 |
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S3063 |
Diclofenac DiethylamineDiclofenac Diethylamine是一种非类固醇消炎药,用于减轻炎症和某些状况下的止痛药。Diclofenac通过抑制COX1和COX2来抑制前列腺素合成,发挥其功能。 |
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S3974 |
(+)-Catechin hydrateCatechins are a plant derived polyphenolic anti-oxidants with phytotoxic properties. (+)-Catechin hydrate is a frequent component of traditional herbal remedies, such as Uncaria rhynchophylla. |
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S4656 |
ParecoxibParecoxib (SC-69124, Valus-P, Vorth-P) 是选择性COX2的抑制剂。 |
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S4609 |
DiflunisalDiflunisal (Dolobid, Dolobis, Flovacil, Fluniget)是水杨酸的二氟苯基衍生物,是非类固醇的消炎药。具有退热、止痛和消炎特性。它是环氧酶抑制剂。 |
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S4176 |
TrometamolTrometamol是一种质子受体,用于治疗酸血症。它能抑制COX1和COX2,因而抑制花生四烯酸向炎性前列腺素的转变。 |
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S5520 |
PhenidonePhenidone (1-phenyl-3-pyrazolidinone), a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), is an organic compound that is primarily used as a photographic developer. |
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S9029 |
Prim-o-glucosylcimifuginPrim-O-glucosylcimifugin (Cimifugin beta-D-glucopyranoside, Cimifugin 7-glucoside) 是防风(Radix Saposhnikovia)中的主要成分,长期以来一直应用于传统中医药中治疗发热、风湿和癌症,它表现出潜在的抗癌活性。在LPS激活的 RAW 264.7 巨噬细胞,Prim-O-glucosylcimifugin 可以浓度依赖性的方式下调 NO synthase (iNOS) 和 cyclooxygenase 2 (COX-2) 的mRNA和蛋白质表达。 |
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S3931 |
Ginsenoside RdGinsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively. |
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S5019 |
IndobufenIndobufen (Ibustrin, K 3920) 是一种可逆的 platelet aggregation 的抑制剂。 Indobufen 是 platelet cyclooxygenase (Cox) 活性的抑制剂,并能抑制凝血恶烷的合成。 |
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S4078 |
Mefenamic AcidMefenamic Acid (CI 473, CN-35355) 是一种竞争性COX-1和COX-2抑制剂。 |
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S4651 |
EtoricoxibEtoricoxib (Arcoxia, MK-663, MK-0663, Tauxib, Algix, Nucoxia)是一种新型的COX-2选择性抑制剂,具有抗炎、退热、止痛和潜在的抗肿瘤活性。 |
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S9386 |
Polygalacic acidPolygalacic acid 是从远志属植物(Polygala paenea L.)分离出的三萜类四羟酸。Polygalacic acid (0-100μM; 24h) 可以显著降低 MMP-3、MMP-9、MMP-13 和 COX-2 的mRNA表达,这些因子的表达由IL-1β诱导可显著增加,并呈现出剂量依赖性。 |
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S4686 |
Vitamin EVitamin E (D-alpha-Tocopherol) 是一种脂溶性的维生素,具有有效的抗氧化特性。它是有效的过氧化氢自由基清除剂并在很多组织中,非竞争性地抑制环氧酶活性。同时通过抑制VEGF基因转录,抑制血管生成和肿瘤休眠。 |
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S6073 |
Diclofenac acidDiclofenac acid是一种非类固醇的消炎药,具有止痛、消炎和退热活性,在治疗多种急性和慢性疼痛、炎症反应中有效。它能抑制cyclooxygenase-1 (COX-1)和cyclooxygenase-2 (COX-2),具有相近的效力。 |
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S4765 |
SyringaldehydeSyringaldehyde (Syringic aldehyde) is an organic compound that occurs naturally in trace amounts. It possesses worthy bioactive properties and is, therefore, used in pharmaceuticals, food, cosmetics, textiles, pulp and paper industries, and even in biological control applications. |
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S5010 |
Indometacin SodiumIndomethacin Sodium (Indometacin Sodium) is the sodium salt of indomethacin, which is a non-selective, reversible, and competitive inhibitor of cyclooxygenases 1 and 2 with anti-inflammatory, analgesic-antipyretic and tocolytic effects. |
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S4230 |
OxaprozinOxaprozin 是一种非麻醉性,非甾体类抗炎药(NSAID),用于缓解与骨关节炎和类风湿关节炎相关的炎症,肿胀,僵硬,关节疼痛。 |
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S5595 |
3-Carene3-Carene (Carene, Delta-3-Carene)是在从松树中提取的精油中的双环单萜。 3-Carene对 COX-2 过表达和LPS诱导的Raw264.7巨噬细胞迁移具有强大的药理作用。3-Carene被证明可显着刺激 alkaline phosphatase 的活性和表达 ,是成骨细胞分化的早期标志。 |
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S2349 |
RutaecarpineRutaecarpine (Rutecarpine) 是从 Evodia rutaecarpa和相关草药中分离的indolopyridoquinazolinone生物碱。是一种新型的COX2抑制剂。 |
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S4360 |
Tolmetin SodiumTolmetin is a non-steroidal anti-inflammatory drug of the arylalkanoic acids. |
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S2351 |
SalicinSalicin (Salicoside, Salicine)是一种醇-β-糖苷,含有D-葡萄糖。是柳树皮产生的一种抗炎剂。它是一种天然的、非选择性的COX1和COX2抑制剂。 |
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S4526 |
FenbufenFenbufen (Lederfen, CL-82204) 是一种具有口服活性的苯基链烷衍生物(phenylalkanoic derivative),它具有抗炎、止痛、解热的活性,是一种非固醇类的消炎药。 |
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S3899 |
HederageninHederagenin (Caulosapogenin, Hederagenol, Hederagenic acid, Astrantiagenin E) is a highly water insoluble triterpenoid compound that can be found in various plants including Hedera helix and Chenopodium quinoa. It exhibits a variety of biological activities, including potent antitumor properties both in vitro and in vivo. Hederagenin inhibits LPS-stimulated expression of iNOS, COX-2, and NF-κB. |
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S5551 |
6-Paradol6-Paradol is a minor constituent of ginger, mainly formed from 6-gingerol via 6-shogaol, and exhibits a variety of biological activities including anti-cancer, anti-inflammatory, and anti-oxidative activities. |
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S9502 |
Madecassic acidMadecassic acid (Brahmic acid) 是最早从积雪草中分离的天然三萜,具有多种消炎和抗糖尿病作用,阻断巨噬细胞中的 NF-κB 活化并导致 iNOS、COX-2、TNF-alpha、IL-1beta 和 IL-6 抑制。 |
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S4539 |
Salicylic acidSalicylic acid (2-Hydroxybenzoic acid)是一种水杨酸,植物中的天然化合物,是乙烯生物合成和环氧酶活性的抑制剂。 |
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S9149 |
BenzoylpaeoniflorinBenzoylpaeoniflorin, a natural product isolated from Chinese paeony root, could inhibit COX-1 and COX-2 in vitro. |
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S6457 |
Flurbiprofen AxetilFlurbiprofen Axetil是一种常用的消炎药,可非特异性地抑制环氧酶COX。 |
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S4509 |
4-Aminoantipyrine4-Aminoantipyrine(Ampyrone, NSC 60242, Metapirazone, Solnapyrin-A, Solvapyrin-A, Minoazophene, Aminoazophene) 是aminopyrine的代谢产物,具有镇痛、消炎退热的效果。Ampyrone刺激肝微粒体,用来测定胞外液。 |
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S3872 |
GuaiacolGuaiacol (O-methoxyphenol, 2-hydroxyanisole, O-methylcatechol) is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. It is a precursor to various flavorants, such as eugenoland vanillin. Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity. |
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S5309 |
Propyphenazone (4-Isopropylantipyrine)Propyphenazone(4-Isopropylantipyrine, Isopropyrine) 是一种止痛退热试剂,一种选择性的 cyclooxygenase-2 抑制剂,具有消炎活性。 |
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S7889 |
XanthohumolXanthohumol,来自啤酒花的一种异戊烯化查耳酮,抑制COX-1和COX-2活性,并表现出化学预防作用。Xanthohumol 可抑制 diacylglycerol acyltransferase 1 (DGAT1) 和 DGAT2,对应的IC50值均为40 μM。Xanthohumol 也是一种有效的针对一系列DNA和RNA病毒的抗病毒药剂。Xanthohumol 在肿瘤细胞中可诱导生长阻滞和凋亡。Phase 1。 |
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S2108 |
Flunixin MegluminFlunixin Meglumin是一种有效的环氧化酶抑制剂,用作镇痛剂,具有抗炎和退热的活性。 |
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S5711 |
DeracoxibDeracoxib (SC-046) is a COX-2 inhibitor with >48-fold selectivity over COX-1. It also exhibits inhibitory activity against phosphodiesterase (Ki = 3.6 μM against human PDE4D3). |
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S3925 |
(-)-Epicatechin gallate(-)-Epicatechin gallate (ECG) 是一种 cyclooxygenase-1 (COX-1) 的抑制剂,IC50值为7.5 μM。 |
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S4295 |
Meclofenamate SodiumMeclofenamate Sodium 是一种双 COX-1/COX-2 抑制剂,其 IC50 分别为40 nM 和 50 nM,用于治疗关节、肌肉疼痛,关节炎以及痛经。Meclofenamate Sodium 是一种非选择性 gap-junction 的阻断剂和高选择性的 fat mass and obesity-associated (FTO) enzyme 抑制剂。 |